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Assay Detail

CHEMBL1785928

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of FGFR1 using poly(Glu-Tyr)4:1 as substrate after 60 mins by ELISA
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 1 (CHEMBL3650)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.
Chen Z, Wang X, Zhu W, Cao X, Tong L, Li H, Xie H, Xu Y, Tan S, Kuang D, Ding J, Qian X.
J Med Chem (2011) 54 : 3732 -3745
PubMed 21517068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.48 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1784734 1 7.72
CHEMBL1784735 1 7.19
CHEMBL1784725 1 7.13
CHEMBL1784736 1 7.11
CHEMBL1784738 1 6.67
CHEMBL1784730 1 6.50
CHEMBL89363 1 6.48
CHEMBL1784742 1 6.37
CHEMBL1784727 1 6.31
CHEMBL1784740 1 6.24
CHEMBL1784729 1 5.68
CHEMBL1784723 1 5.44
CHEMBL1784718 1 5.35
CHEMBL1784722 1 -
CHEMBL1784724 1 -
CHEMBL1784741 1 -
CHEMBL1784726 1 -
CHEMBL1784739 1 -
CHEMBL1784719 1 -
CHEMBL1784737 1 -
CHEMBL1784720 1 -
CHEMBL1784705 1 -
CHEMBL1782083 1 -
CHEMBL1784733 1 -
CHEMBL1784732 1 -
CHEMBL1784731 1 -
CHEMBL1784721 1 -
CHEMBL1784728 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1784734 IC50 = 19.0 nM 7.72
CHEMBL1784735 IC50 = 65.0 nM 7.19
CHEMBL1784725 IC50 = 74.0 nM 7.13
CHEMBL1784736 IC50 = 77.0 nM 7.11
CHEMBL1784738 IC50 = 216.0 nM 6.67
CHEMBL1784730 IC50 = 320.0 nM 6.50
CHEMBL89363 IC50 = 334.0 nM 6.48
CHEMBL1784742 IC50 = 424.0 nM 6.37
CHEMBL1784727 IC50 = 485.0 nM 6.31
CHEMBL1784740 IC50 = 577.0 nM 6.24
CHEMBL1784729 IC50 = 2100.0 nM 5.68
CHEMBL1784723 IC50 = 3600.0 nM 5.44
CHEMBL1784718 IC50 = 4500.0 nM 5.35
CHEMBL1784722 IC50 > 10000.0 nM -
CHEMBL1784724 IC50 > 10000.0 nM -
CHEMBL1784741 IC50 > 10000.0 nM -
CHEMBL1784726 IC50 > 10000.0 nM -
CHEMBL1784739 IC50 > 10000.0 nM -
CHEMBL1784719 IC50 > 10000.0 nM -
CHEMBL1784737 IC50 > 10000.0 nM -
CHEMBL1784720 IC50 > 10000.0 nM -
CHEMBL1784705 IC50 > 10000.0 nM -
CHEMBL1782083 IC50 > 10000.0 nM -
CHEMBL1784733 IC50 > 10000.0 nM -
CHEMBL1784732 IC50 > 10000.0 nM -
CHEMBL1784731 IC50 > 10000.0 nM -
CHEMBL1784721 IC50 > 10000.0 nM -
CHEMBL1784728 IC50 > 10000.0 nM -